CLP-3094

GPR142 is highly expressed in the pancreas and immune system and shares 33% homology with GPR1391. Endogenous agonists identified to date include aromatic amino acids such as tryptophan and phenylalanine2. CLP-3094 was identified as a potent and selective GPR142 antagonist with an IC50=2.3 M against 1 mM L-tryptophan. It inhibited insulin secretion from islets induced by L-tryptophan and other agonists and displayed anti-inflammatory activity in a mouse arthritis model.3